ATE425177T1 - REDUCED FK228 AND ITS USE - Google Patents

REDUCED FK228 AND ITS USE

Info

Publication number
ATE425177T1
ATE425177T1 AT01947940T AT01947940T ATE425177T1 AT E425177 T1 ATE425177 T1 AT E425177T1 AT 01947940 T AT01947940 T AT 01947940T AT 01947940 T AT01947940 T AT 01947940T AT E425177 T1 ATE425177 T1 AT E425177T1
Authority
AT
Austria
Prior art keywords
reduced
salt
compound
histone deacetylase
diseases
Prior art date
Application number
AT01947940T
Other languages
German (de)
Inventor
Hidenori Nakajima
Akito Tanaka
Minoru Yoshida
Sueharu Horinouchi
Original Assignee
Astellas Pharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astellas Pharma Inc filed Critical Astellas Pharma Inc
Application granted granted Critical
Publication of ATE425177T1 publication Critical patent/ATE425177T1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K11/00—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K11/02—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof cyclic, e.g. valinomycins ; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Glass Compositions (AREA)
  • Materials For Medical Uses (AREA)

Abstract

The present invention relates to reduced FK228 of the formula (I) <CHEM> wherein R<1> and R<2> are the same or different and each is a hydrogen atom or a thiol-protecting group, or a salt thereof, and a histone deacetylase inhibitor containing this compound, an expression potentiator and a reactivation promoter of a transgene, and pharmaceutical agents containing them as active ingredients. The reduced FK228 or a salt thereof has a strong histone deacetylase inhibitory activity and this compound can be used for the prophylaxis or treatment of various diseases, in which histone deacetylation is involved, and for the gene therapy of such diseases.
AT01947940T 2000-07-17 2001-07-09 REDUCED FK228 AND ITS USE ATE425177T1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2000216584 2000-07-17

Publications (1)

Publication Number Publication Date
ATE425177T1 true ATE425177T1 (en) 2009-03-15

Family

ID=18711825

Family Applications (1)

Application Number Title Priority Date Filing Date
AT01947940T ATE425177T1 (en) 2000-07-17 2001-07-09 REDUCED FK228 AND ITS USE

Country Status (7)

Country Link
US (1) US7056884B2 (en)
EP (1) EP1302476B1 (en)
JP (1) JP4810784B2 (en)
AT (1) ATE425177T1 (en)
DE (1) DE60137932D1 (en)
ES (1) ES2321584T3 (en)
WO (1) WO2002006307A1 (en)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1313872A1 (en) 2000-09-01 2003-05-28 Fujisawa Pharmaceutical Co., Ltd. A method of producing fr901228
JP4238728B2 (en) * 2001-08-21 2009-03-18 アステラス製薬株式会社 Medicinal uses of histone deacetylase inhibitors and methods for evaluating their antitumor effects
DE60331297D1 (en) 2002-03-07 2010-04-01 Univ Delaware METHOD OF REINFORCING THE OLIGONUCLEOTIDE-mediated NUCLEIC ACID SEQUENCE CHANGE USING HYDROXYAL COMPOSITION COMPOSITIONS
CA2481466A1 (en) * 2002-04-05 2003-10-16 Yoshinori Naoe Depsipeptide for therapy of kidney cancer
JP4804004B2 (en) * 2002-08-20 2011-10-26 アステラス製薬株式会社 Articular cartilage extracellular matrix degradation inhibitor
CA2519320A1 (en) * 2003-02-19 2004-09-02 Astellas Pharma Inc. Method of estimating antitumor effect of histone deacetylase inhibitor
JP2006520796A (en) * 2003-03-17 2006-09-14 タケダ サン ディエゴ インコーポレイテッド Histone deacetylase inhibitor
EP1491188A1 (en) * 2003-06-25 2004-12-29 G2M Cancer Drugs AG Topical use of valproic acid for the prevention or treatment of skin disorders
PT2238982E (en) * 2003-06-27 2013-01-22 Astellas Pharma Inc Therapeutic agent for soft tissue sarcoma
EP2263694B1 (en) * 2003-09-25 2013-06-12 Astellas Pharma Inc. Antitumor agent comprising the histone deacetylase inhibitor FK228 and the topoisomerase II inhibitor doxorubicin
EP1713460A2 (en) * 2003-12-10 2006-10-25 Wisconsin Alumni Research Foundation Fk228 analogs and their use as hdac-inhibitors
US20050137234A1 (en) * 2003-12-19 2005-06-23 Syrrx, Inc. Histone deacetylase inhibitors
WO2005065681A1 (en) * 2003-12-19 2005-07-21 Takeda San Diego, Inc. N- hydroxy-3-(3-(1h-imidazol-2-yl)-phenyl)-acrylamide derivatives and related compounds as histone deacetylase (hdac) inhibitors for the treatment of cancer
US7951780B2 (en) 2004-02-25 2011-05-31 Astellas Pharma Inc. Antitumor agent
US20050187148A1 (en) * 2004-02-25 2005-08-25 Yoshinori Naoe Antitumor agent
JP2008520682A (en) * 2004-11-17 2008-06-19 ザ ユニヴァーシティー オヴ シカゴ Histone deacetylase inhibitors and methods of use thereof
EP1824831A2 (en) * 2004-12-16 2007-08-29 Takeda San Diego, Inc. Histone deacetylase inhibitors
JP2008540574A (en) * 2005-05-11 2008-11-20 タケダ サン ディエゴ インコーポレイテッド Histone deacetylase inhibitor
GB0511266D0 (en) * 2005-06-02 2005-07-13 Trust Chemical compounds
BRPI0613429A2 (en) * 2005-07-14 2009-02-10 Takeda San Diego Inc histone deacetylase inhibitors
JP2009519224A (en) * 2005-11-18 2009-05-14 グロスター ファーマシューティカルズ， インコーポレイテッド Metabolite derivatives of HDAC inhibitor FK228
WO2007084390A2 (en) * 2006-01-13 2007-07-26 Takeda San Diego, Inc. Histone deacetylase inhibitors
CA2650520A1 (en) 2006-04-24 2008-01-31 Gloucester Pharmaceuticals Treatment of ras-expressing tumors
WO2007146730A2 (en) 2006-06-08 2007-12-21 Gloucester Pharmaceuticals Deacetylase inhibitor therapy
US8865655B2 (en) 2006-11-22 2014-10-21 Karus Therapeutics Limited Depsipeptides and their therapeutic use
WO2008083288A2 (en) 2006-12-29 2008-07-10 Gloucester Pharmaceuticals Purifiction of romidepsin
AU2007342030B2 (en) * 2006-12-29 2013-08-15 Celgene Corporation Romidepsin-based treatments for cancer
CA2741265A1 (en) * 2008-10-24 2010-04-29 Gloucester Pharmaceuticals Cancer therapy
JP6049614B2 (en) 2010-07-12 2016-12-21 セルジーン コーポレイション Romidepsin solid forms and their use
US8859502B2 (en) 2010-09-13 2014-10-14 Celgene Corporation Therapy for MLL-rearranged leukemia
WO2013182662A1 (en) * 2012-06-06 2013-12-12 Bionor Immuno As Vaccine
AU2013202506B2 (en) 2012-09-07 2015-06-18 Celgene Corporation Resistance biomarkers for hdac inhibitors
AU2013202507B9 (en) 2012-11-14 2015-08-13 Celgene Corporation Inhibition of drug resistant cancer cells
CN104450837B (en) * 2013-09-18 2019-01-01 上海医药工业研究院 It is a kind of for producing the method and fermentation medium of romidepsin
NZ630311A (en) 2013-12-27 2016-03-31 Celgene Corp Romidepsin formulations and uses thereof
CN109796521B (en) * 2017-11-17 2022-04-19 上海医药工业研究院 Romidepsin acetate crystal form and preparation method thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8817743D0 (en) * 1988-07-26 1988-09-01 Fujisawa Pharmaceutical Co Fr901228 substance & preparation thereof
CA2149038C (en) 1993-09-10 2000-06-13 Motoo Yamasaki Phospholipase c-inhibiting peptides

Also Published As

Publication number Publication date
EP1302476A4 (en) 2006-06-28
JP4810784B2 (en) 2011-11-09
WO2002006307A1 (en) 2002-01-24
EP1302476A1 (en) 2003-04-16
US20040053820A1 (en) 2004-03-18
US7056884B2 (en) 2006-06-06
ES2321584T3 (en) 2009-06-09
EP1302476B1 (en) 2009-03-11
DE60137932D1 (en) 2009-04-23

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